| Cas No.: | 1187020-80-9 |
| Chemical Name: | Lumateperone Tosylate |
| Synonyms: | lumateperone (Tosylate);ITI-007;ITI 007;Lumateperone(ITI-007);lumateperone Tosylate;JIE88N006O;Lumateperone tosylate (USAN);Lumateperone tosylate [USAN];ITI007;Caplyta (TN);D11170;Q27281520;Lumateperone tosylate |
| SMILES: | O=C(NCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCCCCCCCCC(N4CCN(C(C5=CC(CC6=NNC(C7=C6C=CC=C7)=O)=CC=C5F)=O)CC4)=O |
| Formula: | C31H36FN3O4S |
| M.Wt: | 565.6987 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Lumateperone Tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM). IC50 value: 0.54 nM (Ki, for 5-HT2A receptor )Target: 5-HT2A receptorLumateperone also possesses affinity for the D1 receptor (Ki = 52 nM) and weak affinity for the α1A- and α1B-adrenergic receptors (Ki = 173 nM at α1) and D4 receptor. Lumateperone does not significantly bind to the 5-HT2B, 5-HT2C, H1, or mACh receptors. Lumateperone shows a 60-fold difference in its affinities for the 5-HT2A and D2 receptors, which is far greater than that of most or all existing atypical antipsychotics, such as risperidone (12-fold), olanzapine (12.4-fold), and aripiprazole (0.18-fold).[1]in vivo: It is thought that this property may improve the effectiveness and reduce the side effect profile of Lumateperone relative to currently-available antipsychotics, a hypothesis which is supported by the observation of minimal catalepsy in mice treated with Lumateperone.[1] |
| References: | [1]. Lumateperone |
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| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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